This invention relates to an aminoethanesulfonic acid-containing preparation. More particularly, the invention relates to the preparation to be absorbed via the oral or nasal mucosa with a noticeably increased absorption rate of aminoethanesulfonic acid (drug name: xe2x80x9cTaurinexe2x80x9d) in the body. The present invention also relates to a method for absorbing aminoethanesulfonic acid via the oral or nasal mucosa, as well as a method for quick recovery from fatigue, using the said preparation.
Aminoethanesulfonic acid has been known to activate cells and strengthen various organs such as cardiac muscle, cholecyst or liver, and thus to be effective for keeping skin healthy and beautiful and preventing a hangover. Moreover, the acid is said to have an arteriosclerosis-preventing action, because it promotes secretion of bile, increases digestion and absorption of fats and fat-soluble vitamins and inhibits bad cholesterol.
Various kinds of aminoethanesulfonic acid-containing preparations such as injections, drinkable preparations, tablets or powders are now on the market, relying on the development of excellent actions of aminoethanesulfonic acid as depicted above.
Apart from the injections for medicinal purpose, other preparations are intended for oral administration in which aminoethanesulfonic acid is absorbed via the digestive tracts such as the stomach or the intestines.
A considerably longer time is needed for absorption of aminoethanesulfonic acid via the gastrointestinal tracts. Moreover, aminoethanesulfonic acid is unstable to strong acids such as gastric juice or other digestive juices, owing to the primary amino group involved therein, and absorption efficiency of the acid is not satisfactory. With more quick and increased absorption of aminoethanesulfonic acid, one can expect a quick recovery from fatigue after hard exercise or long-range desk work or an earlier recovery of hangover or drunken sickness after heavy drinking.
An object of the present invention is to provide an aminoethanesulfonic acid-containing preparation having an improved absorption rate and absorption efficiency in the body.
We have made our earnest studies to accomplish the above-mentioned object and, as a result, noticed that absorption rate and absorbed amount of aminoethanesulfonic acid is remarkably increased by absorbing it via the oral or nasal mucosa which have been activated by a mucosal stimulant, upon which the invention has been completed.
This invention is directed to a preparation to be applied to the oral or nasal cavity which contains aminoethanesulfonic acid and a mucosal stimulant.
The preparation may include a preparation which contains spices as a mucosal stimulant; it also includes a preparation in the form of chewing gums, troches, pills or aqueous sprays.
This invention includes a method for absorbing aminoethanesulfonic acid in the body via the oral or nasal mucosa by administering the above-mentioned preparation.
The invention further includes a method for quick recovery of fatigue by applying the above-mentioned preparation to the oral or nasal cavity.
The preparation to be applied to the oral or nasal cavity according to the present invention contains aminoethanesulfonic acid and a mucosal stimulant.
Aminoethanesulfonic acid is one of physiologically active substances found in mammals, fish, mollusks and others, which is represented by the general formula H2NCH2CH2SO3H, and which has been marketed in the generic drug name of xe2x80x9cTaurinexe2x80x9d.
The mucosal stimulant is a substance approved as a medicine or food additive, which may stimulate the oral or nasal mucosa to facilitate the blood flow in the intramucosal or submucosal capillaries, and which would not adversely affect a human body. Mucosal stimulants may include spices or herbs; bitters comprising, for example, sodium, potassium, calcium or magnesium salts; natural or synthetic sweeteners such as sucrose, fructose, glucose, milk sugar, sorbitol, maltose, lactose or saccharin sodium; sour substances such as citric acid, malic acid, tartaric acid, fumaric acid, acetic acid or cinnamic acid; flavors comprising esters of such sour substances; aromatic substances such as 1-menthol, anethole, eugenol, cineole, methyl salicylate, spearmint oil, peppermint oil, lemon oil or orange oil; and activating substances such as ethanol or glycerol.
The preparation according to the invention comprises at least one of these mucosal stimulants, preferably several of them.
The dosage forms of the present preparation are not particularly critical, but they may be preferably of the dosage form which could retain the preparation in the oral or nasal cavity as long as possible without swallowing at one gulp. As preparations to be applied to the oral cavity, there may be mentioned, for example, pills (taffies or candies), chewing gums, troches, sublingual tablets, sprays and the like, and chewing gums are particularly preferred. As preparations to be applied to the nasal mucosa, there may be mentioned sprays.
The preparations according to the invention may further contain other additives such as dyes, coloring agents, preservatives, penetrating agents, pH adjusters and the like, as required. There may be also incorporated necessary binding agents, excipients, disintegrating agents, lubricants, gum bases, fillers, emulsifying agents and the like, depending on the dosage forms.
Typically, sugar and starch syrup may be used for candy-like pills. For troches or sublingual tablets, there may be used binding agents such as microcrystalline cellulose, acacia, tragacanth gum or gelatin; excipients such as starch, lactose or carboxymethylcellulose; disintegrating agents such as alginic acid, primogel (sodium starch glycolate) or corn starch; lubricants such as magnesium stearate or sterotex (hydrogenated vegetable oil); glidants such as colloidal silicon dioxide. For chewing gum preparations, there may be used gum base materials such as chicle, jelutong (jelutong gum), sorva (sorva latex), vinyl acetate resins or natural wax, e.g., rice wax, carnaba wax or micro wax; fillers such as calcium carbonate or talc; emulsifying agents such as fatty acid glycerol esters or sugar esters. In addition to water, pH adjusters, solution-stabilizers or sol-stabilizers may be used for sprays for which aerosol forms or pump spraying systems may be adopted.
By applying the preparation according to the invention to the oral or nasal cavity, aminoethanesulfonic acid may be rapidly transferred into blood capillaries and thereafter into the cardiovascular system via the oral or nasal mucosa which has been activated by the action of the mucosal stimulant prior to swallowing. In applying the preparation of the invention to the oral or nasal cavity, in particular, the oral cavity, absorption efficiency of aminoethanesulfonic acid may be increased by retaining it in the oral cavity over a certain period of time without swallowing at one gulp.
For recovery from physical fatigue after exercise or eyestrain caused by desk work, the preparation of the invention may be applied to the oral or nasal cavity to achieve quick recovery from physical fatigue or sleepiness. Also, the said preparation may be applied for sobering up or for the purpose of beauty or medical care.